Assay Detail
Binding
CHEMBL2353183
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Inhibition of human BACE1 using MR121-labeled substrate incubated for 4 mins prior to substrate addition measured after 2 mins by spectrophotometric analysis
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.24 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2347198 | — | — | 1 | 8.22 |
| CHEMBL2347208 | — | — | 1 | 7.92 |
| CHEMBL2347188 | — | — | 1 | 7.89 |
| CHEMBL2347197 | — | — | 1 | 7.89 |
| CHEMBL2347212 | — | — | 1 | 7.85 |
| CHEMBL2347211 | — | — | 1 | 7.80 |
| CHEMBL2347192 | — | — | 1 | 7.77 |
| CHEMBL2347187 | — | — | 1 | 7.72 |
| CHEMBL2347202 | — | — | 1 | 7.72 |
| CHEMBL2347215 | — | — | 1 | 7.64 |
| CHEMBL2347196 | — | — | 1 | 7.60 |
| CHEMBL2347210 | — | — | 1 | 7.58 |
| CHEMBL2347193 | — | — | 1 | 7.58 |
| CHEMBL2347195 | — | — | 1 | 7.57 |
| CHEMBL2347204 | — | — | 1 | 7.55 |
| CHEMBL2347364 | — | — | 1 | 7.50 |
| CHEMBL2347201 | — | — | 1 | 7.44 |
| CHEMBL2347189 | — | — | 1 | 7.40 |
| CHEMBL2347191 | — | — | 1 | 7.38 |
| CHEMBL2347190 | — | — | 1 | 7.31 |
| CHEMBL2347203 | — | — | 1 | 7.29 |
| CHEMBL2347365 | — | — | 1 | 7.29 |
| CHEMBL2347206 | — | — | 1 | 7.27 |
| CHEMBL2347366 | — | — | 1 | 7.24 |
| CHEMBL2347214 | — | — | 1 | 7.18 |
| CHEMBL2347194 | — | — | 1 | 7.17 |
| CHEMBL2347186 | — | — | 1 | 7.11 |
| CHEMBL2347363 | — | — | 1 | 7.06 |
| CHEMBL2347368 | — | — | 1 | 6.97 |
| CHEMBL2347209 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2347198 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2347208 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2347197 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2347188 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2347212 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2347211 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2347192 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2347187 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2347202 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2347215 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2347196 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2347210 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2347193 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2347195 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2347204 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2347364 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2347201 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2347189 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2347191 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2347190 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2347203 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2347365 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2347206 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2347366 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2347214 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2347194 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2347186 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL2347363 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL2347368 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL2347209 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL2347200 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL2347367 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL2347213 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL2347205 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL2347199 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL2347207 | — | IC50 | = | 776.0 | nM | 6.11 |
| CHEMBL2347369 | — | IC50 | = | 41200.0 | nM | 4.38 |